1007882-04-3Relevant academic research and scientific papers
The Discovery of Conformationally Constrained Bicyclic Peptidomimetics as Potent Hepatitis C NS5A Inhibitors
Kazmierski, Wieslaw M.,Miriyala, Nagaraju,Johnson, David K.,Baskaran, Sam
, p. 1649 - 1655 (2021/10/04)
HCV NS5A inhibitors are the backbone of directly acting antiviral treatments against the hepatitis C virus (HCV). While these therapies are generally highly curative, they are less effective in some specific HCV patient populations. In the search for broader-acting HCV NS5A inhibitors that address these needs, we explored conformational restrictions imposed by the [7,5]-azabicyclic lactam moiety incorporated into daclatasvir (1) and related HCV NS5A inhibitors. Unexpectedly, compound 5 was identified as a potent HCV genotype 1a and 1b inhibitor. Molecular modeling of 5 bound to HCV genotype 1a suggested that the use of the conformationally restricted lactam moiety might have resulted in reorientation of its N-terminal carbamate to expose a new interaction with the NS5A pocket located between amino acids P97 and Y93, which was not easily accessible to 1. The results also suggest new chemistry directions that exploit the interactions with the P97-Y93 site toward new and potentially improved HCV NS5A inhibitors.
NOVEL BENZIMIDAZOLE DERIVATIVES
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Paragraph 0187, (2020/01/22)
The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
DICARBAMATE INHIBITORS OF NS5A FOR TREATMENT OF HEPATITIS C VIRUS INFECTIONS AND RELATED DISEASES
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Page/Page column 46; 47, (2020/11/03)
Dicarbamate compounds as inhibitors of NS5A, and therapeutic uses and methods of preparation thereof, are disclosed. These compounds, and pharmaceutically acceptable salts, stereoisomers, tautomers, solvates, and prodmgs, and pharmaceutical compositions t
Monoglycosyl-containing heterocyclic compound for inhibiting hepatitis C viruses and preparation method
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Paragraph 0091-0093, (2019/03/28)
The invention discloses a monoglycosyl-containing heterocyclic compound for inhibiting hepatitis C viruses and a preparation method. The monoglycosyl-containing heterocyclic compound has a chemical structure represented by a formula I shown in the description. The monoglycosyl-containing heterocyclic compound disclosed by the invention can be used for effectively inhibiting protease of the hepatitis C viruses and treating infection of the hepatitis C viruses (HCV).
5,5-FUSED ARYLENE OR HETEROARYLENE HEPATITIS C VIRUS INHIBITORS
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Paragraph 0240; 0241; 0243, (2018/08/20)
Provided herein are 5,5-fused heteroarylene hepatitis C virus inhibitor compounds, for example, of Formula I, IA, or IB, pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host in need thereof.
Preparation method of imidazole ring compound
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Paragraph 0044; 0045; 0050; 0054; 0058-0060; 0062-0064, (2018/12/05)
The invention provides a preparation method of an imidazole ring compound, and belongs to the field of pharmaceutical and chemical industry. The method comprises the following steps: mixing a w material with an organic solvent, a bromination reagent and a
Method for preparing imidazole ring intermediate
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Paragraph 0051; 0052; 0053; 0056, (2018/11/22)
The invention provides a method for preparing an imidazole ring intermediate and belongs to the field of pharmaceutical and chemical industries. The method disclosed by the invention comprises the following steps: carrying out a condensation reaction on s
PROCESS FOR THE PREPARATION OF CARBAMIC ACID, N,N'-[[1,1'-BIPHENYL] -4,4'-DIYLBIS]- 1 H-IMIDAZOLE-5,2 DIYI-(2S)-2,1-PYRROLIDINEDIYL[(1 S)-1-(1-METHYLETHYL)-2-OXO-2,1-ETHANEDIYL]]] BIS-,C,C'-DIMETHYL ESTER AND ITS SALTS AND POLYMORPHS
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Page/Page column 31-32, (2018/08/20)
The present invention relates to the process for the preparation of carbamic acid, N,N'-[[1,1'biphenyl]- 4,4'-diylbis[ I H-imidazole-5,2-diyl-(2S)-2, 1-pyrrolidinediyl[ (1S)-1-( 1-methylethyl)-2- oxo-2,1-ethanediyl]]]bis-,C,C'-dimethyl ester of formula (I
Hepatitis C virus inhibitors
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Page/Page column 179-180, (2017/07/06)
The present invention discloses compounds of Formula (I), and pharmaceutically acceptable salts, esters, or prodrugs thereof: [in-line-formulae]Q-G-A-L-B—Z—W??(I),[/in-line-formulae] which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
HEPATITIS C VIRUS INHIBITORS AND USES THEREOF IN PREPARATION OF DRUGS
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Paragraph 0188; 0190, (2017/12/17)
A series of hepatitis C virus (HCV) inhibitors and compositions and applications thereof in the preparation of drugs for treating chronic HCV infection. Especially, a series of compounds that are used as NS5A inhibitors, and compositions and uses thereof in the preparations of drugs.
